الإشراف على رسائل الماجستير

  SYNTHESIS OF ACETYLCHOLINESTRASE INHIBITOR AS POTENTIAL DRUG FOR THE TREATMENT OF ALZHEIMERʼS
نوع المشرف
مشرف مشارك
تاريخ الاشراف على الرسالة من
الى
اسم الطالب
Fatimah Fathi Alkharaz
ملخص الرسالة
Alzheimer's disease (AD) is a neurodegenerative disorder in which the death of brain cells causes memory loss and cognitive decline. The disease starts with mild symptoms and gradually becomes severe. AD is one of the leading causes of mortality worldwide. Several different hallmarks of the disease have been reported such as low levels of acetylcholine, deposits of β-amyloid around neurons, hyperphosphorylated tau protein, oxidative stress, etc. Strategies for prevention of AD through non pharmacological treatments are associated with lifestyle interventions such as exercise, mental challenges, and socialization as well as caloric restriction and a healthy diet. Pharmacotherapy for AD currently depends on using acetylcholinesterase inhibitors (AChEIs) and N-methyl-D-aspartate (NMDA) receptor antagonists. They provide only symptomatic relief and mostly targets cognitive revival. Quinazoline ring scaffold represents a privileged structure that has been utilized to design therapeutic agents for a wide number of diseases. In this research novel quinazoline derivatives 3 and 4 were synthesized starting from 1-N-Methylisatoic anhydride (1) and different analytical methods were utilized for monitoring and characterization as TLC, GC-MS and NMR (H1 and C13 ) . NH3 was reacted with compound 1 to produce compound 2 giving (85.71%) yield, this product it has been used to synthesis novel compound 3 through the reaction with cycloheptanone catalyzed by toluene-4-sulfonic acid monohydrate afforded the desired compound (97%) yield. The second novel compound 4 was formed through activation of carbonyl carbon in the amide group of 3 with TMSCl followed by reduction with LiAlH4 giving (73.1%) yield. In this work, the reaction conditions were optimized for the synthesis of 3 and 4 allowing to get them in an excellent yield.